Synthesis and pharmacological evaluation of N'-morpholinomethylurea derivatives with platelet antiaggregant activity.
In the attempt to prolong and stabilize the known antiaggregant activity of morpholinomethylurea (MMU) derivatives were prepared with carboxylic acids possessing antiaggregant, anti-inflammatory or hypolipemic activity. The results of the experiments showed the important anti-aggregant and hypolipemic activity of N-2-(p-chlorophenoxy)-isobutyryl-N'-morpholinomethylurea (plafibride, ITA 104). The results obtained seem to indicate that the activity of these new N-acyl-N'-MMU is due initially to the molecule per se although it cannot be totally ruled out that part of the pharmacodynamic effect of the MMU may depend on a prodrug-like behaviour.
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis; D016718:Arachidonic Acid; D001095:Arachidonic Acids / Q000378:metabolism; D055598:Chemical Phenomena; D002621:Chemistry; D002994:Clofibrate / Q000031:analogs & derivatives*; D002995:Clofibric Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D000960:Hypolipidemic Agents / Q000138:chemical synthesis; D066298:In Vitro Techniques; D007928:Lethal Dose 50; D010974:Platelet Aggregation / Q000187:drug effects*; D051381:Rats; D011919:Rats, Inbred Strains
D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001095:Arachidonic Acids; D000960:Hypolipidemic Agents; D016718:Arachidonic Acid; D002995:Clofibric Acid; C016894:plafibride; D002994:Clofibrate